pH依赖-缓释型美沙拉秦结肠靶向小丸的制备与体外评价  

Preparation and Evaluation of pH-Dependent and Sustained-release Pellets for Mesalazine Colon Targeted Delivery

作　　者：傅崇东[1] 徐惠南[1] 张瑜 

机构地区：[1]复旦大学药学院药剂学教研室,上海200032

出　　处：《中国医药工业杂志》2000年第12期541-544,共4页Chinese Journal of Pharmaceuticals

摘　　要：以肠溶型和渗透型丙烯酸树脂为包衣材料制备 p H依赖 -缓释型美沙拉秦结肠靶向小丸 ,评价其体外释放特性。结果表明 ,包衣小丸在 0 .1mol/ L HCl中 2 h几乎不释放药物 ,在 p H7.5缓冲液中具有较好的缓释作用。在模拟胃肠道各区段最高的和最低的 p H变化的释放度试验中 ,均在对应小肠区段时开始缓慢释药 ,分别有 40 %和70 %的药物进入结肠后释放 ,优于单独的肠溶或缓释制剂。The pH-dependent and sustained-release pellets for colon targeted delivery of mesalazine were prepared with the acrylic resin Eudragit S/L and Eudragit RS/RL as coating polymers, and their in vitro release was evaluated. Results indicated that in 0.1 mol/L HCl the pellets released little drug within 2 h, in pH7.5 phosphate buffer the pellets showed sustained-release behavior. With the mimicked release tests of high pH and low pH profile, the release from coated pellets was initiated in the small bowel, and about 40% and 70% of the drug would be released to colon region, respectively. The pellets of this study are superior to formulations coated simply with either enteric polymer or sustained-release polymer.\;

关 键 词：美沙拉秦 结肠靶向小丸 缓释剂 抗溃疡药 

分 类 号：R944.9[医药卫生—药剂学] R975.6[医药卫生—药学]